-
公开(公告)号:US20060235019A1
公开(公告)日:2006-10-19
申请号:US10515434
申请日:2003-05-23
Applicant: Rustum Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith
Inventor: Rustum Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith
IPC: A61K31/53 , A61K31/525 , A61K31/519 , C07D487/02 , C07D475/02
CPC classification number: C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure of Formulas (IA), (IB), or (IC): where the values of the variable are defined herein.
Abstract translation: 提供了能够作为MC4-R激动剂的各种低分子量含胍基分子。 该化合物可用于治疗MC4-R介导的疾病。 化合物具有式(IA),(IB)或(IC)的结构:其中变量的值在本文中定义。
-
公开(公告)号:US20050124597A1
公开(公告)日:2005-06-09
申请号:US10503401
申请日:2003-02-03
Applicant: Rustum Boyce , Daniel Chu , David P. Lentini
Inventor: Rustum Boyce , Daniel Chu , David P. Lentini
CPC classification number: C07K5/06165 , A61K38/00 , C07K5/06139
Abstract: A variety of small, guanidino group-containing molecules capable of acting as MC4-R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4-R mediated diseases and may be formulated into pharmaceutical formulations and compositions.
Abstract translation: 提供了能够作为MC4-R激动剂的各种含有胍基的小分子。 化合物具有本文提供的各种结构。 该化合物可用于治疗MC4-R介导的疾病,并且可以配制成药物制剂和组合物。
-
公开(公告)号:US20060030573A1
公开(公告)日:2006-02-09
申请号:US11248040
申请日:2005-10-11
Applicant: Rustum Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
Inventor: Rustum Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC: A61K31/519 , A61K31/517 , C07D239/88 , C07D403/02 , C07D487/02
CPC classification number: C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.
Abstract translation: 提供了能够作为MC4-R激动剂的各种低分子量含胍基分子。 该化合物可用于治疗MC4-R介导的疾病。 化合物具有结构IA,IB或IC,其中变量的值在本文中定义。
-
公开(公告)号:US07456183B2
公开(公告)日:2008-11-25
申请号:US10474331
申请日:2002-04-08
Applicant: Daniel Chu , Rustum Boyce , David Duhl , Bryan Chang
Inventor: Daniel Chu , Rustum Boyce , David Duhl , Bryan Chang
IPC: A61K31/47 , A61K31/425 , A61K31/415 , A61K31/40 , A61P7/00 , C07D209/02 , C07D209/44 , C07D209/46 , C07D209/48 , C07D217/22 , C07D235/24 , C07D235/28 , C07D277/62 , C07D403/02
CPC classification number: C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10
Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
Abstract translation: 提供具有一般结构I的化合物。 X和Y独立地选自CH 2,N,NR 9,CO,CS,SO,SO 2,S ,(O) - (CR 6),(O) - (CR 6) C(-S) - (CR 6 R 7)N O>,和C(-S) - (CR 6) 其中n为1,2或3.W选自(式I),L选自N,O,SO,SO 2, C(O),NC(O),NC(S),OC(O),OC(S),C(NR 10) ,和共价键。 Z 1,Z 2,Z 3和Z 3独立地选自取代的碳和氮。 式I化合物是黑皮质素-4受体(“MC-4r2”)的激动剂,因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。
-
公开(公告)号:US20050124652A1
公开(公告)日:2005-06-09
申请号:US10503392
申请日:2003-02-03
Applicant: Rustum Boyce , Daniel Chu
Inventor: Rustum Boyce , Daniel Chu
IPC: A61P3/04 , A61P3/10 , C07D209/08 , C07D215/08 , C07D217/06 , C07D217/14 , C07D221/10 , C07D223/16 , C07D401/04 , C07D401/06 , A61K31/47 , A61K31/165 , A61K31/198 , A61K31/277
CPC classification number: C07D209/08 , C07D215/08 , C07D217/06 , C07D217/14 , C07D221/10 , C07D223/16 , C07D401/04 , C07D401/06
Abstract: A variety of small, guanidino group-containing molecules capable of acting as MC4-R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4-R mediated diseases and may be formulated into pharmaceutical formulations and compositions.
Abstract translation: 提供了能够作为MC4-R激动剂的各种含有胍基的小分子。 化合物具有本文提供的各种结构。 该化合物可用于治疗MC4-R介导的疾病,并且可以配制成药物制剂和组合物。
-
公开(公告)号:US20050059662A1
公开(公告)日:2005-03-17
申请号:US10850967
申请日:2004-05-21
Applicant: Rustum Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher Conlee , Brian Thompson , Judith Kuntz , David Musso , Kevin Barvian , Stephen Thomson , William Swain , Kien Du , Brian Chauder , Jason Speake , Michael Bishop
Inventor: Rustum Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher Conlee , Brian Thompson , Judith Kuntz , David Musso , Kevin Barvian , Stephen Thomson , William Swain , Kien Du , Brian Chauder , Jason Speake , Michael Bishop
IPC: A61K31/517 , A61K31/519 , A61K31/525 , A61K31/53 , A61P3/04 , A61P3/10 , C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D475/02 , C07D487/02 , C07D487/04
CPC classification number: C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
Abstract: A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein.
Abstract translation: 提供了能够作为MC4-R激动剂的各种小分子,含胍分子。 当给予受试者时,这些化合物可用于治疗MC4-R介导的疾病。 化合物具有结构IA,IB和IC,其中变量的值在本文中定义。
-
公开(公告)号:US20050038027A1
公开(公告)日:2005-02-17
申请号:US10818187
申请日:2004-04-05
Applicant: Rustum Boyce , David Duhl
Inventor: Rustum Boyce , David Duhl
IPC: C07D401/12 , A61K31/496 , A61K31/519 , A61K31/53 , A61P3/04 , A61P3/10 , A61P7/00 , A61P43/00 , C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10 , C07D403/12 , C07D487/02 , C07D491/02 , A61K31/498 , A61K31/503 , C07D498/02
CPC classification number: C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10
Abstract: Compounds having the general structure III are provided: where D is N or C; W is selected from Z1, Z2, and Z3 are independently selected from CR8 and N; and the other variables have the values described herein. Compounds of formula III have useful properties for controlling diseases related to MC4-R action in humans including obesity and type II diabetes.
Abstract translation: 提供具有通式III的化合物:其中D是N或C; W选自Z 1,Z 2和Z 3独立地选自CR 8和N; 并且其他变量具有本文所述的值。 式III化合物具有用于控制与包括肥胖和II型糖尿病在内的人类MC4-R作用有关的疾病的有用性质。
-
公开(公告)号:US20130017196A1
公开(公告)日:2013-01-17
申请号:US13613977
申请日:2012-09-13
Applicant: Weibo Wang , Paul A. Barsanti , Yia Xia , Rustum Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
Inventor: Weibo Wang , Paul A. Barsanti , Yia Xia , Rustum Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
IPC: A61K31/4174 , C07D401/12 , A61K31/454 , C07D403/12 , A61K31/496 , A61K31/4439 , C07D405/12 , A61K31/4178 , C07D417/12 , A61K31/427 , C07D413/12 , A61K31/422 , A61K31/5377 , C07D498/10 , A61P35/00 , A61K31/4745 , A61K31/7068 , A61K39/395 , A61K33/24 , A61K31/664 , A61P35/02 , C07D233/64
CPC classification number: C07D233/54 , C07D233/24 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/10
Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:
Abstract translation: 本发明涉及新的取代的咪唑化合物及其药学上可接受的盐,酯或前药,新化合物的组合物和药学上可接受的载体,以及新化合物的用途。 本发明的化合物具有以下通式:
-
公开(公告)号:US20110003791A1
公开(公告)日:2011-01-06
申请号:US12882473
申请日:2010-09-15
Applicant: Rustum Boyce , Eric Martin , Weibo Wang , Hong Yang , Paul A. Barsanti
Inventor: Rustum Boyce , Eric Martin , Weibo Wang , Hong Yang , Paul A. Barsanti
IPC: A61K31/553 , A61K31/4178 , A61K31/422 , A61K31/5355 , A61K31/5377 , A61K31/496 , A61K31/551 , A61P35/00 , C12N5/09
CPC classification number: C07D403/06 , C07D413/06
Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:
Abstract translation: 本发明涉及具有下式(I)的新的取代咪唑化合物及其药学上可接受的盐,酯或前药与化合物与药学上可接受的载体的组合物,以及该化合物的用途:
-
公开(公告)号:US06960582B2
公开(公告)日:2005-11-01
申请号:US10426937
申请日:2003-04-30
Applicant: Rustum Boyce , David Duhl
Inventor: Rustum Boyce , David Duhl
IPC: C07D401/12 , A61K31/496 , A61K31/519 , A61K31/53 , A61P3/04 , A61P3/10 , A61P7/00 , A61P43/00 , C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10 , C07D403/12 , C07D487/02 , A61K31/5375 , C07D413/12
CPC classification number: C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10
Abstract: Compounds having the general structure II are provided: A is selected from the group consisting of C or CH and X and Y are independently selected from the group consisting of CH2, N, C═O, C═S, (CR6R7)n, S═O, SO2, O, NR9, S, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n where n is 1, 2, or 3. W is selected from the group consisting of and Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Compounds of formula II are agonists of the melanocortin-4 receptor (“MC4-R”) and therefore may have useful properties for controlling diseases related to MC4-R action in humans, such as obesity and type II diabetes.
Abstract translation: 提供具有通式II的化合物:A选自C或CH,X和Y独立地选自CH 2,N,CO,CS,(CR SO 2,SO 2,O,NR 9,SO 3,SO 2,SO 2, ,(C) - (CR) - (CR 6) - (CR 6) 其中n为1,2或3.W选自Z 1,...,S 2,...,N 2, Z 2,Z 3,Z 3,Z 3独立地选自取代的碳和氮。 L选自由N,O,S,SO,SO 2,C(O),NC(O),NC(S),OC(O),OC(S) ,C(NR 10),C(NOR 10)和共价键。 式II化合物是黑皮质素-4受体(“MC4-R”)的激动剂,因此可能具有控制人类MC4-R作用相关疾病如肥胖和II型糖尿病的有用性质。
-
-
-
-
-
-
-
-
-